Delving into the Latest Updates on Eberconazole Nitrate with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Eberconazol, Eberconazole

+ [2]

Target

fungal CYP51A1

Mechanism

fungal CYP51A1 inhibitors(Fungal CYP51A1 inhibitors)

Therapeutic Areas

Infectious DiseasesSkin and Musculoskeletal Diseases

Active Indication

TineaTinea Pedis

Inactive Indication-

Originator Organization

Laboratorios Salvat SA

Active Organization

Laboratorios Salvat SA

Inactive Organization-

Drug Highest PhaseApproved

First Approval Date

ES (01 Jan 2005),

Tinea Pedis

Regulation-

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Structure

Molecular FormulaC18H14Cl2N2

InChIKeyMPTJIDOGFUQSQH-UHFFFAOYSA-N

CAS Registry128326-82-9

View All Structures (2)

BackgroundMultidrug resistant bacterial and fungal pathogens are resistant to a number of significant front-line drugs, hence, identification of new inhibitory agents to combat them is crucial. In this study, we aim to evaluate the activity of Pandemic Box compounds from Malaria Medicines Venture (MMV) against A. baumannii and P. aeruginosa bacterial, C. auris, C. albicans and A. niger fungal clinical isolates.MethodsIsolates were initially screened with 201 antibacterial and 46 antifungal compounds (10 μM) using a microbroth dilution in triplicates to determine MIC. A persister assay was performed for bacterial pathogens.ResultsOut of 201 antibacterial compounds, twenty-nine and seven compounds inhibited the growth of A. baumannii and P. aeruginosa at 10 μM, respectively. MMV1580854, MMV1579788, eravacycline and epetraborole inhibited both the bacterial test isolates. In a persister assay, MMV1634390 showed complete bactericidal effect against A. baumannii. With antifungal activity compounds, C. auris responded to15 compounds, Six compounds inhibited C. albicans and one was effective against A. niger at 10 μM. The ratio of Minimum Fungicidal Concentration (MFC): Minimum Inhibitory Concentration (MIC) of MMV1782110 was 2 against C. auris. Eberconazole, amorolfine and luliconazole are fungicidal targeting C. albicans at a MFC: MIC ratio of 2.ConclusionFive compounds from MMV Pandemic Box were found to be inhibiting colistin and ceftazidime resistant A. baumannii clinical isolate, also against colistin and β-lactam resistant P. aeruginosa clinical isolate. MMV1634390 showed complete bactericidal effect against A. baumannii in a persister assay. MMV1782110, Eberconazole, amorolfine and luliconazole exhibited potent anti-fungal activity. Further investigations are warranted to identify the targets and mechanism.

01 Jan 2023·Drug Research

Development and Evaluation of Topical Ethosomal Gel for Fungal Infections

Article

Author: Hafeez, Abdul ; Gupta, Preeti ; Kushwaha, Poonam

AbstractBackground Fungal infections are one of the most common dermatological issues worldwide. Candida species-caused fungal infections are frequent on the cutaneous surface. Eberconazole (EBZ) has the strongest antifungal action against Candida spp., the major source of fungal infections.Method In the present study, the cold method followed by probe sonication was used to create EBZ-loaded ethosomal dispersion. The solubility of ethosomes in different lipids and surfactants was used to choose these components. Under magnetic stirring, the dispersion was absorbed into a carbopol 934 gel. In vitro antifungal activity was performed using the Agar well diffusion method, and their topical effectiveness against pathogenic Candida albicans was compared to that of a marketed formulation containing EBZ.Results Eberconazol incorporated into gel displayed sustained release in an in vitro release assay. Based on the zone of inhibition diameters, EBZ formulation was determined to be efficient against C. albicans when compared to the commercialized cream and plain gel.Conclusion Based on these findings, the current study found that EBZ possesses significant antifungal efficacy against C. albicans.

01 Sep 2021·Indian Journal of DermatologyQ4 · MEDICINE

Efficacy and Safety of Eberconazole vs Sertaconazole in Localised Tinea Infection

Q4 · MEDICINE

ArticleOA

Author: Munusamy, Rajesh ; Srikanth, S ; Kumar, B Aravinda ; Ravichandran, Mirunalini

Background:Topical antifungals especially azole group of drugs are effective agents in the treatment of dermatophytoses producing 100% clinical and mycological cure. Each of them vary having specific characteristics to tackle several clinical challenges like high relapse rate, recurrences and quality of life.Aims and Objectives:To compare the efficacy and safety of Eberconazole and Sertaconazole in tinea infection.Materials and Methods:This was a randomized, observer-blinded, parallel-group study conducted at a dermatology out-patient department (OPD) of tertiary care teaching hospital in Puducherry. 85 patients with tinea corporis and tinea cruris infections who visited the dermatology OPD were enrolled in this study. The treatment phase involved two groups receiving either Sertaconazole 2% cream or Eberconazole 1% applied topically twice daily for 4 weeks. At the end of treatment phase, there was a 'follow-up phase' at the end of 4 weeks, where the patients were assessed clinically and mycologically. The data were analyzed using descriptive statistics using MS Excel version 2019 and SPSS version 15 for Windows.Results:The primary efficacy variables namely change in pruritus, erythema, induration, scaling and mycological cure significantly improved in both the groups, as compared to baseline (P < 0.001), in the treatment phase and follow-up phase. Intergroup comparison with respect to pruritus and scaling showed significant difference (P < 0.001), suggestive of better reduction of pruritus and scaling scores at 4 weeks with Sertaconazole when compared to Eberconazole.Conclusions:Sertaconazole was better than Eberconazole in relieving signs and symptoms of dermatophytoses, especially pruritus, thereby improving patients' quality of life.

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